Retinoic acid receptor
The retinoic acid receptor (RAR) is a type of nuclear receptor which can also act as a transcription factor[1] that is activated by both all-trans retinoic acid and 9-cis retinoic acid.[2] There are three retinoic acid receptors (RAR), RAR-alpha, RAR-beta, and RAR-gamma, encoded by the RARA, RARB, RARG genes, respectively. Each receptor isoform has several splice variants: four- for alpha, four- for beta, and two- for gamma.
As with other type II nuclear receptors, RAR heterodimerizes with RXR and in the absence of ligand, the RAR/RXR dimer binds to hormone response elements known as retinoic acid response elements (RAREs) complexed with corepressor protein. Binding of agonist ligands to RAR results in dissociation of corepressor and recruitment of coactivator protein that, in turn, promotes transcription of the downstream target gene into mRNA and eventually protein.
See also
References
- ↑ Germain P, Chambon P, Eichele G, Evans RM, Lazar MA, Leid M, De Lera AR, Lotan R, Mangelsdorf DJ, Gronemeyer H (2006). "International Union of Pharmacology. LX. Retinoic acid receptors". Pharmacol Rev. 58 (4): 712–25. doi:10.1124/pr.58.4.4. PMID 17132850.
- ↑ Allenby G, Bocquel MT, Saunders M, Kazmer S, Speck J, Rosenberger M, Lovey A, Kastner P, Grippo JF, Chambon P, Levin AA (1993). "Retinoic acid receptors and retinoid X receptors: interactions with endogenous retinoic acids". Proc Natl Acad Sci USA. 90 (1): 30–4. doi:10.1073/pnas.90.1.30. PMC 45593. PMID 8380496.
External links
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(2) Zinc finger DNA-binding domains |
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| (2.1) Nuclear receptor (Cys4) | subfamily 1 | |
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| subfamily 2 | |
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| subfamily 4 | |
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| subfamily 0 | |
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| (2.2) Other Cys4 | |
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| (2.3) Cys2His2 | |
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| (2.5) Alternating composition | |
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(4) β-Scaffold factors with minor groove contacts |
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(0) Other transcription factors |
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see also transcription factor/coregulator deficiencies |
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CAR | |
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ERR | | |
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- DY-131 (GSK-9089)
- GSK-4716 (GW-4716)
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FXR | |
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LXR | |
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PPAR | | |
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| SPPARMs | |
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| Antagonists |
- FH-535
- GW-9662
- SR-202
- T-0070907
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| Unknown | |
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| Unselective | |
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| Unsorted | |
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PXR | |
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RAR | Agonists | |
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| Antagonists |
- BMS-195614
- BMS-493
- CD-2665
- ER-50891
- LE-135
- MM-11253
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| Others |
- Retinoic acid metabolism inhibitors: Liarozole
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RXR | Agonists | |
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| Antagonists |
- HX-531
- HX-630
- LG-100754
- PA-452
- UVI-3003
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SHR | | See here instead. |
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TR | |
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